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Literature summary for 2.7.11.18 extracted from
- Isoform-specific knockout of endothelial myosin light chain kinase: closing the gap on inflammatory lung disease (2004), Trends Pharmacol. Sci., 25, 64-66.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | therapeutic inhibition via specific chemical inhibitors of endothelial isozyme, i.e. 11-(3-chloro-6-immino-6H-pyridazin-1-yl)-undecanoic acid (6-phenyl-pyridazin-3-yl)-amide, represents an important new target for the treatment of inflammatory lung disease with less side effects than other therapies | Mus musculus |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| additional information | construction of eMLCK or smMLCK knockout mutant mice by genetic or chemical methods, overview | Mus musculus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 11-(3-chloro-6-iminopyridazin-1(6H)-yl)-N-(6-phenylpyridazin-3-yl)undecanamide | highly specific inhibitor, competitive to ATP binding | Mus musculus |  |
| KT5926 | i.e. (8R,9S,11S)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-14-n-propoxy-2,3,9,10-tetrahydro-8,11-epoxy,1H,8H,11H-2,7beta,11alpha-triazadeibenzo[a,g]cycloocta[cde]triden-1-one, specific inhibitor | Homo sapiens | |
| ML-7 | i.e. 1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine HCl, specific inhibitor | Homo sapiens | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 108000 | - |
smooth muscle isozyme | Mus musculus |
| 130000 | 150000 | smooth muscle isozyme | Homo sapiens |
| 210000 | - |
endothelial isozyme | Mus musculus |
| 214000 | - |
endothelial isozyme | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + [myosin light chain] | Mus musculus | - |
ADP + [myosin light chain] phosphate | - |
? | |
| ATP + [myosin light chain] | Homo sapiens | activation of the enzyme is a key regulatory step in the modulation of endothelial permeability, central to parthogenesis of inflammatory lung disease is disruption of the endothelial barrier function | ADP + [myosin light chain] phosphate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
2 isozymes encoded by a single gene and translated from 2 different splicing variants | - |
| Mus musculus | - |
2 isozymes encoded by a single gene and translated from 2 different splicing variants | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| endothelium | specific isozyme | Mus musculus | - |
| endothelium | specific isozyme | Homo sapiens | - |
| smooth muscle | specific isozyme | Mus musculus | - |
| smooth muscle | specific isozyme | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + [myosin light chain] | - |
Mus musculus | ADP + [myosin light chain] phosphate | - |
? | |
| ATP + [myosin light chain] | - |
Homo sapiens | ADP + [myosin light chain] phosphate | - |
? | |
| ATP + [myosin light chain] | activation of the enzyme is a key regulatory step in the modulation of endothelial permeability, central to parthogenesis of inflammatory lung disease is disruption of the endothelial barrier function | Homo sapiens | ADP + [myosin light chain] phosphate | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | the endothelial isozyme possesses a catalytic domain including the actin-binding domain and the calmodulin binding domain, like the smooth muscle isozyme, but also a protein-protein interaction domain including SH2 and SH3 domains | Mus musculus |
| More | the endothelial isozyme possesses a catalytic domain including the actin-binding domain and the calmodulin binding domain, like the smooth muscle isozyme, but also a protein-protein interaction domain including SH2 and SH3 domains | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| endothelial MLCK | - |
Mus musculus |
| endothelial MLCK | - |
Homo sapiens |
| endothelial myosin light chain kinase | - |
Mus musculus |
| endothelial myosin light chain kinase | - |
Homo sapiens |
| MLCK | - |
Mus musculus |
| MLCK | - |
Homo sapiens |
| myosine light chain kinase | - |
Mus musculus |
| myosine light chain kinase | - |
Homo sapiens |
| smMLCK | - |
Mus musculus |
| smMLCK | - |
Homo sapiens |
| smooth muscle myosin light chain kinase | - |
Mus musculus |
| smooth muscle myosin light chain kinase | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Mus musculus | |
| ATP | - |
Homo sapiens | |
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Release 2023.1 (January 2023)
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